Insights into a PCSK9 structural groove: a harbinger of new drugs to reduce LDL-cholesterol

被引：6
|
作者：
Seidah, Nabil G. [1 ]
机构：
[1] Clin Res Inst Montreal, Biochem Neuroendocrinol Lab, Montreal, PQ, Canada
来源：
NATURE STRUCTURAL & MOLECULAR BIOLOGY | 2017年 / 24卷 / 10期
关键词：
PROPROTEIN; MUTATIONS; BINDING; DEGRADATION; PEPTIDE;
D O I：
10.1038/nsmb.3471
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
PCSK9 enhances LDL cholesterol (LDL-c) levels by escorting the liver LDL receptor (LDLR) to endosomes and lysosomes for degradation. PCSK9 monoclonal antibodies and RNA-antisense formulations are effective in reducing LDL cholesterol in patients. The recent structural identification of a novel pocket in PCSK9 paves the way to the future development of orally active small-molecule hypocholesterolemic drugs.
引用
收藏
页码：785 / 786
页数：2
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